An improved automated radiosynthesis of [F-18]FET-beta AG-TOCA
File(s)
Author(s)
Allott, Louis
Barnes, Chris
Brickute, Diana
Aboagye, Eric O
Type
Journal Article
Abstract
The fluorine-18 radiolabelled octreotide derivative [18F]FET-βAG-TOCA targeting somatostatin receptor type 2, has been evaluated clinically for positron emission tomography (PET) imaging of neuroendocrine tumours (NETs). We report an improved automated radiosynthesis of [18F]FET-βAG-TOCA with several advantages over the current automated GMP synthesis: 1) cartridge-based purification of 2-[18F]fluoroethylazide ([18F]FEA); 2) simple set-up for the radiolabelling on a single cassette; 3) HPLC purification using a biocompatible mobile phase. [18F]FET-βAG-TOCA was produced with a radiochemical yield of 16.7 ± 0.6% (non-decay corrected) and radiochemical purity ≥98%. The automated synthesis produced multi-patient doses (900 MBq) that were radiochemically stable (≥98%) over 4 hours. In addition, the automated procedure described can be used, with minimal adaptation, to radiolabel any alkyne-containing peptide with [18F]FEA using the GE FASTlab™ platform.
Date Issued
2019-03-01
Date Acceptance
2018-12-11
Citation
Reaction Chemistry and Engineering, 2019, 4 (3), pp.569-574
ISSN
2058-9883
Publisher
Royal Society of Chemistry
Start Page
569
End Page
574
Journal / Book Title
Reaction Chemistry and Engineering
Volume
4
Issue
3
Copyright Statement
© The Royal Society of Chemistry 2019.
Sponsor
Medical Research Council (MRC)
Medical Research Council (MRC)
Identifier
http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:000459805800006&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=1ba7043ffcc86c417c072aa74d649202
Grant Number
MR/J007986/1
MR/N020782/1
Subjects
Science & Technology
Physical Sciences
Technology
Chemistry, Multidisciplinary
Engineering, Chemical
Chemistry
Engineering
PRECLINICAL EVALUATION
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AZIDE
Publication Status
Published
Date Publish Online
2018-12-11